Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 109a (R)-tert-Butyl 3-Methyl-4-(6-nitropyridin-3-yl)piperazine-1-carboxylate 109a A 100-mL single-neck round-bottomed flask equipped with a magnetic stirrer and reflux condenser was charged with 1,4-dioxane (60 mL), 5-bromo-2-nitropyridine (2.0 g, 10.0 mmol), (R)-tert-butyl 3-methylpiperazine-1-carboxylate (2.0 g, 10.0 mmol), and cesium carbonate (6.5 g, 20 mmol). See . After bubbling nitrogen through the resulting mixture for 30 minutes, XantPhos (579 mg, 1.0 mmol) and tris(di-benzylideneacetone)dipalladium(0) (915 mg, 1.0 mmol) were added, and the reaction mixture was heated at 100 C. for 15 h. After this time the reaction was cooled to room temperature and filtered. The filtrate was partitioned between ethyl acetate (100 mL) and water (100 mL). The aqueous layer was separated and extracted with ethyl acetate (150 mL*3). The combined organic layer was washed with brine (50 mL) and dried over sodium sulfate. The drying agent was removed by filtration and the filtrate was concentrated under reduced pressure. The residue was purified on flash column eluting with 30:1 DCM/MeOH to afford 109a (1.6 g, 44%) as a yellow solid. MS: [M+H]+ 323. 1H NMR (500 MHz, DMSO) delta 8.21 (d, J=3.5, 1H), 8.18 (d, J=9.0, 1H), 7.43-7.45 (m, 1H), 4.33 (s, 1H), 3.92-3.99 (m, 1H), 3.80 (d, J=12.5, 2H), 3.06-3.23 (m, 3H), 1.43 (s, 9H), 1.09 (d, J=6.5, 3H).

163765-44-4, 163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GENENTECH, INC.; Crawford, James John; Young, Wendy B.; US2013/116245; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21416-67-1, 4,4′-(Propane-1,2-diyl)bis(piperazine-2,6-dione) is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

At the beginning of each working day the capillary was flushed with NaOH 0.1M for 10min, 5min with Milli-Q water and 40min with the buffer in basic conditions and with MeOH for 5min, NaOH 1M for 25min, 5 min with Milli-Q water, 5min with HCl 0.1M and 30min with the buffer in acid conditions. In order to ensure the repeatability between injections, the capillary was flushed with NaOH 0.1M for 5min, 5min with the buffer and 2min with the BGE in basic or acid conditions. Buffer solutions were prepared by dissolving the appropriate amount of formic acid, acetic acid, ammonium bicarbonate or boric acid in Milli-Q water, adjusting the pH to the desired value (pH 2.5, 5.0, 7.0, or 9.0, respectively) with 0.1 or 1M NaOH before completing the volume with water to get the desired buffer concentration. Finally, BGEs were prepared by dissolving the appropriate amount of the chiral selectors in the buffer solution. Stock standard solutions of racemic captopril, econazole and clenbuterol were prepared by dissolving the appropriate amount of these drugs in MeOH and razoxane was prepared by dissolving the appropriate amount in Milli-Q water/25% DMF (v/v). These solutions were stored at 4C. All solutions (buffers and standards) were filtered through 0.45mum pore size nylon membrane filters before their injection in the CE system., 21416-67-1

The synthetic route of 21416-67-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Quintana, Sara; Garcia, Maria Angeles; Marina, Maria Luisa; Gomez, Rafael; de la Mata, F. Javier; Ortega, Paula; Tetrahedron Asymmetry; vol. 28; 12; (2017); p. 1797 – 1802;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a mixture of 4-(4-carboxy-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (250 mg, 0.82 mmol) and 2-aminothiazole (125 mg, 0.83 mmol) in DMF (20 mL) was added EDCl (184 mg, 0.96 mmol) and DMAP (100 mg, 0.83 mmol). The mixture was stirred at room temperature overnight and then heated to 100 C. for 5 hrs. Solvents were evaporated and the residue was extracted with ethyl acetate and ammonium chloride solutions. The residue was crystallized from methanol (40 mL) to afford the intermediate 4-[4-(benzothiazol-2-ylcarbamoyl)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester. LCMS calc for C23H26N4O3S (m/e) 438.17, obsd 439.2 (M+H).The above intermediate was then suspended in methylene chloride (3 mL) and treated with trifluoroacetic acid (1 mL). The mixture was stirred at room temperature for 1 hr and then the solvents were evaporated. The residue was dried, triturated with ether and filtered to afford N-benzothiazol-2-yl-4-piperazin-1-yl-benzamide trifluoroacetate (130 mg) MS calc for C18H18N4OS (m/e) 338., obsd 339. (M+H)

162046-66-4, The synthetic route of 162046-66-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Bolin, David Robert; Cheung, Adrian Wai-Hing; Hamilton, Matthew Michael; Marcopulos, Nicholas; McDermott, Lee Apostle; Qian, Yimin; US2010/113782; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,31166-44-6

Step 1 Preparation of Compound 132To a suspension of NaOt-Bu (3.73 g, 38.9 mmol), Pd(dba)2 (0.298 g, 0.518 mmol), RuPhos (0.484 g, 1.036 mmol) and 2-bromo-l,4-difluorobenzene (5 g, 25.9 mmol) in Toluene (50 ml) was added benzyl piperazine-l-carboxylate (6.00 ml, 31.1 mmol) at r.t. under N2.The mixture was stirred at 100¡ãC under N2 for 1 hr. The reaction mixture was diluted with H20 and AcOEt at r.t., then the resulting solid was filtered, rinsed with AcOEt and H2O.The filtrate was extracted with AcOEt x 2. The organic layers were combined and washed with brine. The organic layer was dried over MgS04, filt and cone. The crude product was added to a silica gel column and was eluted with AcOEt-Hexane. Collected fractions were evaporated. The residual oil was triturated with CH2C12-Hexane, then filtered, rinsed with Hexane to afford compound 132 (3.7 g, 43.0 percent) as a white solid.1H-NMR (CDC13) delta: 7.40-7.29 (5H, m), 7.01-6.89 (1H, m), 6.66-6.56 (2H, m), 5.16 (2H, s), 3.67 (4H, t, J= 5.1 Hz), 3.11-2.97 (4H, m).

As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference£º
Patent; Shionogi & Co., Ltd.; KUROSE, Noriyuki; WO2011/162409; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

INTERMEDIATE 5 (S)-(4-Methyl-piperazin-2-yl)-methanolTo a stirred suspension of (S)-piperazine-l,3-dicarboxylic acid l-tert-buty ester (5.00 g, 21.7 mmol) in THF (40 mL) was slowly added 1.0 M borane-THF complex solution (32.6 rnL, 32.6 mmol). The reaction was heated to 90 0C and stirred under reflux for 2 hours. The reaction mixture was removed from the heat before a further 1.5 equivalents of 1.0 M borane-THF complex solution (32.6 mL, 32.6 mmol) was added. The reaction was reheated to 90 0C and stirred under reflux for a further 2 hours. The reaction was cooled to 0 0C and quenched by the slow addition of MeOH. The reaction mixture was then concentrated in vacuo. The white solid obtained was dissolved in THF (30 mL), cooled to 0 0C and slowly added a 2.0M solution of LiAlH4 in THF (27 mL, 54.0 mmol). The reaction was heated to 90 0C and stirred under reflux for 2h. A further portion of 2.0M solution of LiAlH4 in THF (27 mL, 54.0mmol) was added and the reaction stirred under reflux for 4h and then at room temperature overnight. The reaction mixture was cooled to O0C and quenched by the slow addition of 1.0M aq NaOH solution until the exothermic reaction subsided. The resulting gel was diluted with THF and the solids filtered off. The filtrate was then concentrated in vacuo to afford (S)-(4-methyl-piperazin-2-yl)-methanol (2.84 g, 101% crude yield) as a colourless oil., 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BIOVITRUM AB (PUBL); WO2009/71658; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

5-(4-Fluorophenyl)-5-methyl-3-(oxiran-2-ylmethyl)imidazolidine-2,4-dione 17 (3.5 mmol, 1.2 eq) with appropriate piperazine derivative (3.0 mmol, 1.0 eq) in 50 mL flat-bottom flask were irradiated in household microwave: 300 MW (1 min), 450 MW (1 min), 300 MW (2 min). Progress of reaction was controlled by TLC (DCM/MeOH 95:5). Pure products were obtained from crude glue-reactants after microwave reaction by: crystallization from methanol (Method A), column chromatography with DCM/MeOH (98:2) as eluent (Method B) and/or dissolving in ethanol and saturating with gaseous HCl to provide product in form of hydrochloride (Method C)., 115761-79-0

As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference£º
Article; Kucwaj-Brysz, Katarzyna; Warszycki, Dawid; Podlewska, Sabina; Witek, Jagna; Witek, Karolina; Izquierdo, Andrea Gonzalez; Sata?a, Grzegorz; Loza, Maria I.; Lubelska, Annamaria; Latacz, Gniewomir; Bojarski, Andrzej J.; Castro, Marian; Kie?-Kononowicz, Katarzyna; Handzlik, Jadwiga; European Journal of Medicinal Chemistry; vol. 112; (2016); p. 258 – 269;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3-fluoro-4- (N-t-butoxycarbonylpiperazin-1-yl) aniline (16.8 g, 57 mmol) (obtained according to the procedure described in preparation 3) in THF (30 ml), dimethyl aniline (7.92 ml, 62. 7 mmol) was added. To this benzyl chloroformate (8.27 ml, 58. 14 mmol) dissolved in THF (20 ml) was added over a period of 20 min upon stirring at 0 C. After completion of the reaction, the resulting mixture was quenched with saturated NaCl solution (50 ml) and extracted with EtOAc (3 x 200 ml). The organic layer was evaporated, dried over Na2S04 and purified using silica gel column using 50% EtOAc in hexane to afford the title compound (24 g).

154590-35-9, 154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Orchid Chemicals &amp Pharmaceuticals Ltd; WO2004/18439; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.954388-33-1,(R)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.,954388-33-1

Step 1. 1 -benzyl 4-tert-butyl f2R)-2-[(2.2,2-trifluoroethyl)carbamoyl]piperazine-L4- dicarboxylateA solution of (R)~N-4-BOC-N-l-CBZ-piperazine carboxylic acid (4.0 g, 11 mmol), 2,2,2-trifluoroethyiamine hydrochloride (1.78 g, 13 mmol), EDC (2.74 g, 14 mmol), HOBt (1.68 g, 11 mmol) and Hunig’s base (5.75 mL, 33 mmol) in DCM (100 mL) was stirred at ambient temperature for 18 h. The reaction mixture was washed with aqueous 5% sodium bicarbonate (100 mL) and brine. The organic layer was dried over sodium sulfate, filter and concentrated in vacuo. The residue was purified by silica gel chromatography, eluting with a gradient of 5 – 70 % ethyl acetate in hexane, to afford the title compound as white foam. MS APCI: [M + Na]+ m/z – 468.0.

954388-33-1 (R)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid 6558854, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; CASH, Brandon; FISCHER, Christian; GARCIA, Yudith; JUNG, Joon; KATZ, Jason; KIM, June; RIVKIN, Alexey; SCHELL, Adam; SIU, Tony; WITTER, David; ZHOU, Hua; WO2011/137022; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A 100 mL round-bottom flask was charged with 2-chloro-4-(morpholin-4- yl)benzaldehyde (0.800 g, 3.54 mmol, 1.00 equiv), tert-butyl (2S)-2-methylpiperazine-l- carboxylate (0.783 g, 3.91 mmol, 1.10 equiv) , 1,2-dichloroethane (20 mL). The mixture was stirred for 30 min at room temperature. Sodium triacetoxyborohydride (2.26 g, 10.7 mmol, 3.00 equiv) was added. The resulting solution was stirred overnight at room temperature, diluted with ]0 (30 mL), extracted with dichloromethane (3 x 30 mL) and the organic layers were combined, dried over Na2S04, filtered and concentrated under reduced pressure. The residue was chromatographed on a silia gel column with ethyl acetate/petroleum ether (25/75) to provide 1.20 g (74% yield) of tert-butyl (2S)-4-[[2-chloro-4-(morpholin-4- yl)phenyl]methyl]-2-methylpiperazine-l-carboxylate as a white solid. LCMS (ESI, m/z): 410 [M+H]+., 169447-70-5

Big data shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; ABIDE THERAPEUTICS; THE SCRIPPS RESEARCH INSTITUTE; CISAR, Justin, S.; GRICE, Chery, A.; JONES, Todd, K.; NIPHAKIS, Micah, J.; CHANG, Jae, Won; LUM, Kenneth, M.; CRAVATT, Benjamin, F.; WO2013/103973; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Intermediate 46: 1,1-dimethylethyl (3S)-3-(hydroxymethyl)-4-(trifluoroacetyl)-1-piperazinecarboxylate 1,1-dimethylethyl (3S)-3-(hydroxymethyl)-1-piperazinecarboxylate (Commercial) (350 mg, 1.618 mmol) was dissolved in Dichloromethane (DCM) (10 ml) and cooled in an ice bath under nitrogen. Triethylamine (0.564 ml, 4.05 mmol) was added followed by the careful addition of trifluoroacetic anhydride (0.571 ml, 4.05 mmol). After ?10 mins, the ice bath was removed and the reaction was allowed to warm to room temperature and stirred for 3 hours. The reaction was washed with water. The aqueous was extracted with DCM. The combined organics were washed with water, dried using a hydrophobic frit and evaporated in vacuo to give a pale yellow oil (0.69 g) LCMS (Method B): Rt=0.45 min, MH+=245, 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; Atkinson, Francis Louis; Atkinson, Stephen John; Barker, Michael David; Douault, Clement; Garton, Neil Stuart; Liddle, John; Patel, Vipulkumar Kantibhai; Preston, Alexander G.; Shipley, Tracy Jane; Wilson, David Matthew; Watson, Robert J.; US2014/5188; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics